Delving into the Latest Updates on CGP-35949 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

CysLT

Mechanism

CysLT antagonists(Cysteinyl leukotriene receptor antagonists)

Therapeutic Areas

Immune System DiseasesRespiratory Diseases

Active Indication-

Inactive Indication

Asthma

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis Pharma AG

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC23H26ClN5O5

InChIKeyKOMGKDHFTYYZRF-UHFFFAOYSA-N

CAS Registry103448-74-4

The effects of CGP 33304 and CGP 35949 were studied in standardized model of traumatic shock. Both drugs are dual leukotriene receptor antagonists and phospholipase A2 inhibiting agents. Pentobarbital anesthetized rats (35 kg/mg) subjected to Noble-Collip drum trauma were characterized by a 128 +/- 16 min survival time and a 4-fold increase in plasma myocardial depressant factor (MDF) activity. CGP 33304 and CGP 35949 both significantly (p less than 0.01) attenuated the accumulation of MDF activity in the plasma (24 +/- 3 and 29 +/- 3 U/ml, respectively, vs. 57 +/- 5 U/ml in the trauma and vehicle group). A significant improval in survival time (p less than 0.05) was observed in the CGP 33304 treated group (182 +/- 23 min) and the CGP 35949 treated group (204 +/- 33 min). Both drugs exhibited significant anti-proteolytic activity in pancreatic homogenates. CGP 33304 and CGP 35949 appear to attenuate MDF production, probably secondary to their anti-proteolytic effect and the improved state of the splanchnic circulation. Both drugs also may prevent hypoxia secondary to leukotriene induced bronchoconstriction in shock states. CGP 33304 and CGP 35949 may, therefore, prove to be useful therapeutic agents in acute ischemic disorders including traumatic shock.

01 Jan 1987·Advances in prostaglandin, thromboxane, and leukotriene research

CGP 35949: a potent leukotriene antagonist and inhibitor of phospholipase. Biological profile.

Article